Nifedipine nanocrystals: pharmacokinetic evaluation in the rat and permeability studies in Caco-2/HT29-5M21 (co)-cultures

Hecq, Julien; Nollevaux, Géraldine; Deleers, Michel; Fanara, D.; Vranckx, Henri; Peulen, Olivier; Dandrifosse, Guy; Amighi, Karim

doi:10.1016/s1773-2247(06)50084-x

Cited by 9 publications

(2 citation statements)

References 26 publications

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“…The concentration of nifedipine in plasma was measured by HPLC method. Briefly, 100 µL plasma samples and 10 µL of 20 µg/mL internal standard nimodipine were stirred for 30 s, 10 µL of 1 mol/L NaOH was then added into the sample with stirring for 1 min [23]. The analytes were extracted from the samples with 1 mL of diethyl ether/chloroform (5:1 v/v) by vortex mixing for 5 min.…”

Section: Pharmacokinetic Studymentioning

confidence: 99%

A Liposomal Formulation for Improving Solubility and Oral Bioavailability of Nifedipine

et al. 2020

Molecules

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Proliposomes were used to improve the solubility and oral bioavailability of nifedipine. Nifedipine proliposomes were prepared by methanol injection-spray drying method. The response surface method was used to optimize formulation to enhance the encapsulation efficiency (EE%) of nifedipine. The particle size of nifedipine proliposomes after rehydration was 114 nm. Surface morphology of nifedipine proliposomes was observed by a scanning electron microscope (SEM) and interaction of formulation ingredients was assessed by differential scanning calorimetry (DSC). The solubility of nifedipine is improved 24.8 times after forming proliposomes. In vitro release experiment, nifedipine proliposomes had a control release effect, especially in simulated gastric fluid. In vivo, nifedipine proliposomes significantly improved the bioavailability of nifedipine. The area under the concentration-time curve (AUC0–∞) of nifedipine proliposomes was about 10 times than nifedipine after oral administration. The elimination half-life (T1/2β) of nifedipine was increased from 1.6 h to 6.6 h. In conclusion, proliposomes was a promising system to deliver nifedipine through oral route and warranted further investigation.

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Section: Pharmacokinetic Studymentioning

confidence: 99%

A Liposomal Formulation for Improving Solubility and Oral Bioavailability of Nifedipine

et al. 2020

Molecules

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“…However, animal models have shown that mebudipine's oral bioavailability is very low (4), which is similar to the oral bioavailability of similar compounds, such as nimodipine (5), nitrendipine (6), nicardipine (7), and nifedipine (8). Slow rates of dissolution and extensive first-pass effects cause the low oral bioavailability of these dihydropyridines.…”

Section: Introductionmentioning

confidence: 99%

Improved Oral Bioavalability of Mebudipine Upon Administration in PhytoSolve and Phosal-Based Formulation (PBF)

Khani

Keyhanfar

2013

AAPS PharmSciTech

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The aim of this investigation was to examine the efficacy of PhytoSolve and Phosal-based formulation (PBF) to enhance the oral bioavailability of mebudipine, which is a poorly water-soluble calcium channel blocker. The solubility of mebudipine in various oils was determined. PhytoSolve was prepared with a medium-chain triglyceride (MCT) oil (20%), soybean phospholipids (5%), and a 70% fructose solution (75%). The influence of the weight ratio of Phosal 50PG to glycerol in PBF on the mean globule size was studied with dynamic light scattering. The optimized formulation was evaluated for robustness toward dilution, transparency, droplet size, and zeta potential. The in vivo oral absorption of different mebudipine formulations (PhytoSolve, PBF, oily solution, and suspension) were evaluated in rats. The optimized PBF contained Phosal 50PG/glycerol in a 6:4 ratio (w/w). The PBF and PhytoSolve formulations were miscible with water in any ratio and did not demonstrate any phase separation or drug precipitation over 1 month of storage. The mean particle size of PhytoSolve and PBF were 138.5 ± 9.0 and 74.4 ± 2.5 nm, respectively. The in vivo study demonstrated that the oral bioavailability of PhytoSolve and PBF in rats was significantly higher than that of the other formulations. The PhytoSolve and PBF formulations of mebudipine are found to be more bioavailable compared with suspension and oily solutions during an in vivo study in rats. These formulations might be new alternative carriers that increase the oral bioavailability of poorly water-soluble molecules, such as mebudipine.

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Nanosuspensions

Burgess

2011

Long Acting Injections and Implants

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Nifedipine nanocrystals: pharmacokinetic evaluation in the rat and permeability studies in Caco-2/HT29-5M21 (co)-cultures

Cited by 9 publications

References 26 publications

A Liposomal Formulation for Improving Solubility and Oral Bioavailability of Nifedipine

A Liposomal Formulation for Improving Solubility and Oral Bioavailability of Nifedipine

Improved Oral Bioavalability of Mebudipine Upon Administration in PhytoSolve and Phosal-Based Formulation (PBF)

Nanosuspensions

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